cyproterone acetate [Ligand Id: 2865] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL139835 (SH-714, Cyproterone, Androcur 10, Cyprostat, Androcur, Cyproterone Acetate, Diane, NSC-81430)
  • A1 receptor/Adenosine A1 receptor in Rat [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
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  • Androgen receptor/Androgen Receptor in Human [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275]
  • Androgen receptor/Androgen Receptor in Rat [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207]
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  • μ receptor/Mu opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
ChEMBL Adenosine A1 receptor binding was measured in adenosine deaminase (ADA) pretreated rat cortical membranes using [3H]cyclohexyladenosine in the presence of 2-chloroadenosine B 8.89 pKi 1.3 nM Ki J. Med. Chem. (1990) 33: 1919-1924 [PMID:2362269]
ChEMBL Binding affinity against adenosine A1 receptor from rat brain membranes using [3H]cyclohexyladenosine as radioligand. B 9.12 pKi 0.76 nM Ki J. Med. Chem. (1992) 35: 2881-2890 [PMID:1495019]
ChEMBL Displacement of [3H]DPCPX from adenosine A1 receptor of rat cortical membranes with GTP B 6.9 pIC50 125 nM IC50 J. Med. Chem. (2004) 47: 2243-2255 [PMID:15084123]
ChEMBL Displacement of [3H]DPCPX from adenosine A1 receptor of rat cortical membranes without GTP B 8.3 pIC50 5 nM IC50 J. Med. Chem. (2004) 47: 2243-2255 [PMID:15084123]
Androgen receptor/Androgen Receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275]
GtoPdb - - 7.85 pKi 14 nM Ki J. Med. Chem. (1998) 41: 623-39 [PMID:9484511]
ChEMBL Binding affinity for human androgen receptor in transiently-transfected COS-1 cells. B 7.85 pKi 14 nM Ki J. Med. Chem. (1998) 41: 623-639 [PMID:9484511]
ChEMBL Antagonistic activity against human androgen receptor (hAR) in co-transfected CV-1 cells. F 7.64 pIC50 23 nM IC50 J. Med. Chem. (1998) 41: 623-639 [PMID:9484511]
Androgen receptor/Androgen Receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207]
ChEMBL DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone) B 7.51 pKi 31 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Inhibition of [3H]-R-1881 binding to rat ventral prostate cytosolic androgen receptor B 4.74 pIC50 18000 nM IC50 J. Med. Chem. (2000) 43: 4629-4635 [PMID:11101354]
ChEMBL Inhibitory concentration against recombinant rat androgen receptor expressed in Escherichia coli using [3H]methyltrienolone (R 1881) B 6.2 pIC50 630.96 nM IC50 J. Med. Chem. (2005) 48: 5666-5674 [PMID:16134935]
ChEMBL DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone) B 7.33 pIC50 47 nM IC50 DrugMatrix in vitro pharmacology data
Glucocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2034] [GtoPdb: 625] [UniProtKB: P04150]
ChEMBL DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone) B 6.99 pKi 102 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone) B 6.65 pIC50 225 nM IC50 DrugMatrix in vitro pharmacology data
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine) B 6.05 pKi 886 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine) B 5.66 pIC50 2183 nM IC50 DrugMatrix in vitro pharmacology data
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay F 5.1 pIC50 7943.28 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
Progesterone receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL208] [GtoPdb: 627] [UniProtKB: P06401]
ChEMBL Antagonistic activity against human progesterone receptor B (hPR-B) in co-transfected CV-1 cells. F 6 pIC50 >1000 nM IC50 J. Med. Chem. (1998) 41: 623-639 [PMID:9484511]
Progesterone receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1909044] [UniProtKB: Q690N0]
ChEMBL DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020) B 8.31 pKi 4.84 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020) B 7.43 pIC50 37 nM IC50 DrugMatrix in vitro pharmacology data

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]